LM22A-4 - Trk Receptor Agonist - 生命科學試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELM22A-4Cat. No.: HY-100673CAS No.: 37988-18-4分式: CHNO分量: 339.34作靶點: Trk Receptor作通路: Neuronal Signaling; Protein Tyrosine Kinase/RTK儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 H2O : 50 mg/mL (

2、147.34 mM)DMSO : 29 mg/mL (85.46 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.9469 mL 14.7345 mL 29.4690 mL5 mM 0.5894 mL 2.9469 mL 5.8938 mL10 mM 0.2947 mL 1.4734 mL 2.9469 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍福渲魄?/p>

3、請先配制澄清的儲備液，再依次添加助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.37 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.37 mM); Clear solution1/3

4、 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.37 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 LM22A-4種特異性的 tyrosine kinase receptor B 激動劑，常于神經(jīng)系統(tǒng)疾病研究。體外研究 LM22A-4 significantly up-regulates OPN and ALPase mRNA expression in a dose-dependent man

5、ner andOC mRNA level is significantly increased by 5 M of LM22A-4. LM22A-4 significantly increases OPN,ALPase and OC mRNA expression in a time-dependent manner. LM22A-4 stimulated OPN and OC mRNAexpression in HCEM cells cultured with mineralizing media 2.體內(nèi)研究 LM22A-4 (10 mg/kg, i.p.) significantly r

6、educes the degree of tissue injury and apoptosis (TUNEL staining andcaspase-3 and Bcl-2 expression) compared with vehicle treated group. LM22A-4 also significantlyameliorates the recovery of limb function. LM22A-4 (10 mg/kg) treatment results in a significant increase inneuron number. LM22A-4 admini

7、stration (10 mg/kg) significantly improves the neurological scores comparedwith those of the solvent-treated animals 1.PROTOCOLAnimal ICR mice are randomly divided into five groups: sham treatment, spinal cord injury, spinal cord injuryAdministration 1 combined with solvent treatment, spinal cord in

8、jury combined with LM22A-4 treatment (10 mg/kg), and spinalcord injury combined with LM22A-4 treatment (15 mg/kg), with each group containing 26 animals.Preparation of the mouse SCI model is based on a previous study and on a protocol employed by this group.Briefly, a mouse is anesthetized via the a

9、dministration of chloral hydrate (4 mg/kg) before a 3-cm incision isintroduced on its back. T7-T11 vertebrae are exposed under a surgical microscope before the laminae areremoved with a vascular clip to fully expose the spinal cord. The spinal cord is clamped with the vascular clipfor 1 minute with

10、a force of 10 g. The animal is then subjected to complete staunching of the bleeding, andthe incised dorsal muscle and skin are sutured. Mice from the control group undergo laminectomy, fullexposure of the spinal cord, and subsequent suturing, but without aortic clamping. After the surgery, the mice

11、are placed on a warm blanket until fully awake and are then housed in cages accommodating a normal diet.After the SCI treatment, 14 mice are sacrificed to enable molecular and histological examinations; the other14 mice are allowed to live for 20 days for neurological scoring and are sacrificed on d

12、ay 20 via cervicaldislocation.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Yu G, et al. Protective effects of LM22A-4 on injured spinal cord nerves. Int J Clin Exp Pathol. 2015 Jun 1;8(6):6526-32. eCollection2015.2. Kajiya M, et al. BDNF mimetic compound LM22A-4 regulates cementoblast differentiation via the TrkB-ERK/Akt signaling cascade. IntImmunopharmacol. 2014 Apr;19(2):245-52.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEMcePdfHeight